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Assay Detail

CHEMBL762563

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Potent effective concentration was evaluated for KATP channel opening activity in pig bladder strips
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Sus scrofa
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Sulfonylurea receptors; K-ATP channels (CHEMBL2095152)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
Turner SC, Carroll WA, White TK, Brune ME, Buckner SA, Gopalakrishnan M, Fabiyi A, Coghlan MJ, Scott VE, Castle NA, Daza AV, Milicic I, Sullivan JP.
Bioorg Med Chem Lett (2003) 13 : 1741 -1744
PubMed 12729655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 6.70 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50760 1 8.05
CHEMBL49153 1 7.31
CHEMBL300958 1 7.28
CHEMBL47170 1 7.09
CHEMBL299167 1 7.02
CHEMBL296840 1 6.90
CHEMBL48848 1 6.74
CHEMBL45749 1 6.69
CHEMBL48797 1 6.52
CHEMBL49806 1 6.43
CHEMBL296931 1 6.41
CHEMBL295458 1 6.37
CHEMBL49035 CROMAKALIM 2.0 1 6.34
CHEMBL300969 1 6.26
CHEMBL49076 1 6.21
CHEMBL49797 1 6.15
CHEMBL301296 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50760 EC50 = 8.913 nM 8.05
CHEMBL49153 EC50 = 48.98 nM 7.31
CHEMBL300958 EC50 = 52.48 nM 7.28
CHEMBL47170 EC50 = 81.28 nM 7.09
CHEMBL299167 EC50 = 95.5 nM 7.02
CHEMBL296840 EC50 = 125.89 nM 6.90
CHEMBL48848 EC50 = 181.97 nM 6.74
CHEMBL45749 EC50 = 204.17 nM 6.69
CHEMBL48797 EC50 = 302.0 nM 6.52
CHEMBL49806 EC50 = 371.54 nM 6.43
CHEMBL296931 EC50 = 389.05 nM 6.41
CHEMBL295458 EC50 = 426.58 nM 6.37
CHEMBL49035 CROMAKALIM EC50 = 457.09 nM 6.34
CHEMBL300969 EC50 = 549.54 nM 6.26
CHEMBL49076 EC50 = 616.6 nM 6.21
CHEMBL49797 EC50 = 707.95 nM 6.15
CHEMBL301296 EC50 = 851.14 nM 6.07